Idraparinux, the fully O-sulfated, O-methylated, heparin-related pentasaccharide possessing selective factor Xa inhibitory activity, was prepared by two novel synthetic pathways. Each route was based on a 2+3 block synthesis utilizing the same l-iduronic acid-containing trisaccharide acceptor, which was glycosylated with either a glucuronide disaccharide donor or its non-oxidized precursor. The latter
通过两种新颖的合成途径制备了具有完全选择性的Xa抑制活性的完全O-
硫酸化,O-甲基化,
肝素相关的五糖Idraparinux 。每种途径均基于使用相同的含1-艾杜糖醛酸的三糖受体的2 + 3嵌段合成,所述三糖受体被
葡糖醛酸二糖供体或其未氧化的前体糖基化。后一种途径涉及以五糖
水平将
葡萄糖单元氧化成d-
葡萄糖醛酸,被证明是更有效的,以合理的总产率提供了目标五糖。